Ulixertinib (BVD-523)
For research use only.
Catalog No.S7854 Synonyms: VRT752271
29 publications
CAS No. 869886-67-9
Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.
Purity & Quality Control
Choose Selective ERK Inhibitors
Biological Activity
| Description | Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Targets |
|
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| In vitro |
In an A375 melanoma cell line containing a b-RAFV600E mutation, Ulixertinib reduces the levels of phosphorylated ERK2 (pERK) and of the phosphorylation of the downstream kinase RSK (pRSK) with IC50 of 4.1/0.14 μM, respectively. Ulixertinib also inhibits A375 cell proliferation with IC50 of 180 nM. [1] |
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Cell Data |
|
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Assay |
|
Protocol
| Kinase Assay:[1] |
- Collapse
ERK2 Rapidfire Mass Spectrometry Inhibition of Catalysis Assay: MEK U911-activated ERK2 protein is expressed and purified in-house. Enzyme and substrate solutions are made up in assay buffer consisting of 50 mM Tris (pH 7.5), 10 mM MgCl2, 0.1 mM EGTA, 10 mM DTT and 0.01% (v/v) CHAPS. 1.2 nM ERK2 protein is prepared in assay buffer and 10 µL is dispensed into each well of a polypropylene, 384-well plate containing test and reference control compounds. The compound plates had previously been dosed with a 12 point range from 100 µM down to 0.1 nM in order to calculate compound IC50s, with a total DMSO concentration in the assay of 1%. Following a 20 minute pre-incubation of enzyme and compound at room temperature, 10 µL of substrate solution is added consisting of 16 µM Erktide (IPTTPITTTYFFFK) and 120 µM ATP (measured Km) in assay buffer. The reaction is allowed to progress for 20 minutes at room temperature before being quenched by the addition of 80 µl 1% (v/v) formic acid. The assay plates are then run on the RapidFire Mass Spectrometry platform to measure substrate (unphosphorylated Erktide) and product (phosphorylated Erktide) levels. |
|---|---|
| Cell Research:[1] |
- Collapse
|
Solubility (25°C)
| In vitro | DMSO | 86 mg/mL (198.46 mM) |
|---|---|---|
| Ethanol | 15 mg/mL (34.61 mM) | |
| Water | Insoluble |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 433.33 |
|---|---|
| Formula | C21H22Cl2N4O2 |
| CAS No. | 869886-67-9 |
| Storage |
powder in solvent |
| Synonyms | VRT752271 |
| Smiles | CC(C)NC1=NC=C(C(=C1)C2=CNC(=C2)C(=O)NC(CO)C3=CC(=CC=C3)Cl)Cl |
In vivo Formulation Calculator (Clear solution)
| Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment) | ||||||||||
| Dosage | mg/kg |  |
Average weight of animals | g | |
Dosing volume per animal | ul | |
Number of animals | |
| Step 2: Enter the in vivo formulation () | ||||||||||
| % DMSO % % Tween 80 % ddH2O | ||||||||||
| CalculateReset | ||||||||||
Calculation results:
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT04488003 | Recruiting | Drug: Ulixertinib|Drug: Physician''s Choice | Advanced Solid Tumor|BRAF Gene Mutation|BRAF Gene Alteration|MEK Mutation|MEK Alteration|MAP2K1 Gene Mutation|MAP2K1 Gene Alteration|MAP2K2 Gene Mutation|MAP2K2 Gene Alteration | BioMed Valley Discoveries Inc | November 3 2020 | Phase 2 |
| NCT04145297 | Recruiting | Drug: Ulixertinib|Drug: Hydroxychloroquine | Gastrointestinal Neoplasms | University of Utah|BioMed Valley Discoveries Inc | March 17 2020 | Phase 1 |
| NCT03698994 | Suspended | Other: Pharmacokinetic Study|Drug: Ulixertinib | Advanced Malignant Solid Neoplasm|Recurrent Ependymal Tumor|Recurrent Ewing Sarcoma|Recurrent Glioma|Recurrent Hepatoblastoma|Recurrent Histiocytic and Dendritic Cell Neoplasm|Recurrent Langerhans Cell Histiocytosis|Recurrent Malignant Germ Cell Tumor|Recurrent Malignant Solid Neoplasm|Recurrent Medulloblastoma|Recurrent Neuroblastoma|Recurrent Non-Hodgkin Lymphoma|Recurrent Osteosarcoma|Recurrent Peripheral Primitive Neuroectodermal Tumor|Recurrent Primary Malignant Central Nervous System Neoplasm|Recurrent Rhabdoid Tumor|Recurrent Rhabdomyosarcoma|Recurrent Soft Tissue Sarcoma|Refractory Ependymoma|Refractory Ewing Sarcoma|Refractory Glioma|Refractory Hepatoblastoma|Refractory Histiocytic and Dendritic Cell Neoplasm|Refractory Langerhans Cell Histiocytosis|Refractory Malignant Germ Cell Tumor|Refractory Malignant Solid Neoplasm|Refractory Medulloblastoma|Refractory Neuroblastoma|Refractory Non-Hodgkin Lymphoma|Refractory Osteosarcoma|Refractory Peripheral Primitive Neuroectodermal Tumor|Refractory Primary Malignant Central Nervous System Neoplasm|Refractory Rhabdoid Tumor|Refractory Rhabdomyosarcoma|Refractory Soft Tissue Sarcoma|Wilms Tumor | National Cancer Institute (NCI) | October 1 2018 | Phase 2 |
| NCT02994732 | Completed | Drug: [14C]-BVD-523 | Healthy | BioMed Valley Discoveries Inc | January 2017 | Phase 1 |
| NCT02296242 | Completed | Drug: BVD-523 | Acute Myelogenous Leukemia|Myelodysplastic Syndrome | BioMed Valley Discoveries Inc | November 2014 | Phase 1|Phase 2 |
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.
